Towards a species-selective acetylcholinesterase inhibitor to control the mosquito vector of malaria, Anopheles gambiae |
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| Authors: | Paul R Carlier Troy D Anderson Dawn M Wong Danny C Hsu Joshua Hartsel Ming Ma Eric A Wong Ranginee Choudhury Polo C-H Lam Maxim M Totrov Jeffrey R Bloomquist |
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| Institution: | aDepartment of Chemistry, Virginia Tech, Blacksburg, VA 24061, USA;bDepartment of Entomology, Virginia Tech, Blacksburg, VA 24061, USA;cDepartment of Animal and Poultry Sciences, Virginia Tech, Blacksburg, VA 24061, USA;dMolsoft LLC, 3366 North Torrey Pines Court, Suite 300, La Jolla, CA 92037, USA |
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| Abstract: | Anopheles gambiae is the major mosquito vector of malaria in sub-Saharan Africa. At present, insecticide-treated nets (ITNs) impregnated with pyrethroid insecticides are widely used in malaria-endemic regions to reduce infection; however the emergence of pyrethroid-resistant mosquitoes has significantly reduced the effectiveness of the pyrethroid ITNs. An acetylcholinesterase (AChE) inhibitor that is potent for An. gambiae but weakly potent for the human enzyme could potentially be safely deployed on a new class of ITNs. In this paper we provide a preliminary pharmacological characterization of An. gambiae AChE, discuss structural features of An. gambiae and human AChE that could lead to selective inhibition, and describe compounds with 130-fold selectivity for inhibition of An. gambiae AChE relative to human AChE. |
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| Keywords: | Acetylcholinesterase Inhibitor Mosquito Human Anopheles Insecticide |
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